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Assay Detail

CHEMBL820190

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Binding
Inhibition of cRaf1 kinase in cascade assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of potent cRaf1 kinase inhibitors.
Lackey K, Cory M, Davis R, Frye SV, Harris PA, Hunter RN, Jung DK, McDonald OB, McNutt RW, Peel MR, Rutkowske RD, Veal JM, Wood ER.
Bioorg Med Chem Lett (2000) 10 : 223 -226
PubMed 10698440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.49 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1794051 1 8.05
CHEMBL1794050 GW429374A 1 7.96
CHEMBL1794052 GW405841X 1 7.89
CHEMBL418892 1 7.80
CHEMBL73554 1 7.75
CHEMBL75988 1 7.60
CHEMBL311402 1 7.54
CHEMBL73470 1 7.50
CHEMBL73157 1 7.40
CHEMBL1789963 GW406108X 1 7.34
CHEMBL72179 1 7.19
CHEMBL75275 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1794051 IC50 = 9.0 nM 8.05
CHEMBL1794050 GW429374A IC50 = 11.0 nM 7.96
CHEMBL1794052 GW405841X IC50 = 13.0 nM 7.89
CHEMBL418892 IC50 = 16.0 nM 7.80
CHEMBL73554 IC50 = 18.0 nM 7.75
CHEMBL75988 IC50 = 25.0 nM 7.60
CHEMBL311402 IC50 = 29.0 nM 7.54
CHEMBL73470 IC50 = 32.0 nM 7.50
CHEMBL73157 IC50 = 40.0 nM 7.40
CHEMBL1789963 GW406108X IC50 = 46.0 nM 7.34
CHEMBL72179 IC50 = 65.0 nM 7.19
CHEMBL75275 IC50 = 1300.0 nM 5.89